ES2309540T3 - 3-fluoropiperidinas como antagonistas de nmda/nr2b. - Google Patents

3-fluoropiperidinas como antagonistas de nmda/nr2b. Download PDF

Info

Publication number: ES2309540T3
Authority: ES; Spain
Prior art keywords: pharmaceutically acceptable; aryl; compound according; baselineskip; compound
Prior art date: 2003-06-04
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Expired - Lifetime

Application number

ES04753896T

Other languages

English (en)

Spanish (es)

Inventor

Nigel J. Liverton

Christopher F. Claiborne

David A. Claremon

John A. Mccauley

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Merck and Co Inc

Original Assignee

Merck and Co Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2003-06-04

Filing date

2004-05-28

Publication date

2008-12-16

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33511734&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2309540(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-05-28 Application filed by Merck and Co Inc filed Critical Merck and Co Inc

2008-12-16 Application granted granted Critical

2008-12-16 Publication of ES2309540T3 publication Critical patent/ES2309540T3/es

2024-05-28 Anticipated expiration legal-status Critical

Status Expired - Lifetime legal-status Critical Current

Links

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/04—Centrally acting analgesics, e.g. opioids
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A—HUMAN NECESSITIES
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- A61P25/22—Anxiolytics
- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
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- A61P25/36—Opioid-abuse
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Neurology (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Virology (AREA)
Addiction (AREA)
Immunology (AREA)
Physical Education & Sports Medicine (AREA)
Rheumatology (AREA)
Oncology (AREA)
Orthopedic Medicine & Surgery (AREA)
Ophthalmology & Optometry (AREA)
Psychology (AREA)
Endocrinology (AREA)
Molecular Biology (AREA)
Communicable Diseases (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Hospice & Palliative Care (AREA)
Tropical Medicine & Parasitology (AREA)
Biotechnology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
AIDS & HIV (AREA)

ES04753896T 2003-06-04 2004-05-28 3-fluoropiperidinas como antagonistas de nmda/nr2b. Expired - Lifetime ES2309540T3 (es)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US47593803P	2003-06-04	2003-06-04
US475938P		2003-06-04

Publications (1)

Publication Number	Publication Date
ES2309540T3 true ES2309540T3 (es)	2008-12-16

Family

ID=33511734

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ES04753896T Expired - Lifetime ES2309540T3 (es)	2003-06-04	2004-05-28	3-fluoropiperidinas como antagonistas de nmda/nr2b.

Country Status (30)

Country	Link
EP (1)	EP1648882B1 (de)
JP (1)	JP3927228B2 (de)
KR (1)	KR20060017839A (de)
CN (1)	CN1798744A (de)
AR (1)	AR044579A1 (de)
AT (1)	ATE403651T1 (de)
AU (1)	AU2004245522B2 (de)
BR (1)	BRPI0410837A (de)
CA (1)	CA2527093C (de)
CL (1)	CL2004001365A1 (de)
CO (1)	CO5700762A2 (de)
DE (1)	DE602004015610D1 (de)
DK (1)	DK1648882T3 (de)
EC (1)	ECSP056192A (de)
ES (1)	ES2309540T3 (de)
HR (1)	HRP20080490T3 (de)
IS (1)	IS8117A (de)
MA (1)	MA27781A1 (de)
MX (1)	MXPA05013151A (de)
MY (1)	MY138547A (de)
NO (1)	NO20060020L (de)
PE (1)	PE20050245A1 (de)
PL (1)	PL1648882T3 (de)
PT (1)	PT1648882E (de)
RU (1)	RU2339630C2 (de)
SI (1)	SI1648882T1 (de)
TW (1)	TW200510378A (de)
UA (1)	UA81319C2 (de)
WO (1)	WO2004108705A1 (de)
ZA (1)	ZA200509000B (de)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20090285862A1 (en) *	2006-05-03	2009-11-19	Cnsbio Pty Ltd.	Methods and composition for treatment of inflammatory pain
MX2009011416A (es) *	2007-04-23	2009-11-05	Janssen Pharmaceutica Nv	Tia(di)azoles como antagonistas del receptor de dopamina 2 de disociacion rapida.
WO2009000038A1 (en) *	2007-06-28	2008-12-31	Cnsbio Pty Ltd	Combination methods and compositions for treatment of neuropathic pain
CA2788656A1 (en)	2010-02-16	2011-08-25	Pfizer Inc.	(r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors
KR20140146217A (ko)	2012-04-20	2014-12-24	유씨비 파마, 에스.에이.	파킨슨병을 치료하는 방법
CN103936663B (zh) *	2013-01-23	2016-12-28	艾琪康医药科技（上海）有限公司	一种1-r1-3,3-二氟(或3-氟)-4-r2-4-氨甲基哌啶及其衍生物的制备方法
US9221796B2 (en)	2014-01-09	2015-12-29	Bristol-Myers Squibb Company	Selective NR2B antagonists
US9187506B2 (en)	2014-01-09	2015-11-17	Bristol-Myers Squibb Company	(R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders
TW201609741A (zh)	2014-06-04	2016-03-16	盧郡控股（開曼）有限公司	作為ｎｒ２ｂｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物
RU2017107558A (ru)	2014-09-15	2018-10-18	Руджен Холдингс (Кайман) Лимитед	Производные пирролопиримидина в качестве антагонистов nmda-рецептора nr2b
WO2016049048A1 (en) *	2014-09-22	2016-03-31	Rugen Holdings (Cayman) Limited	Treatment of anxiety disorders and autism spectrum disorders
US10202363B2 (en) *	2014-12-23	2019-02-12	Cerecor, Inc.	Compounds, compositions and methods
US10221182B2 (en)	2015-02-04	2019-03-05	Rugen Holdings (Cayman) Limited	3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists
KR102613179B1 (ko) *	2015-06-01	2023-12-14	뤼겐 홀딩스 (케이맨) 리미티드	Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물
BR112018007181A2 (pt)	2015-10-14	2018-10-16	Bristol-Myers Squibb Company	antagonistas de nr2b seletivos
KR20180063306A (ko)	2015-10-14	2018-06-11	브리스톨-마이어스 스큅 컴퍼니	선택적 nr2b 길항제
TWI732031B (zh)	2016-08-31	2021-07-01	日商衛材R&D企管股份有限公司	吡唑并[1, 5-a]嘧啶化合物
US11000526B2 (en)	2016-11-22	2021-05-11	Rugen Holdings (Cayman) Limited	Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
PL364625A1 (en) *	2001-02-23	2004-12-13	Merck & Co, Inc.	N-substituted nonaryl-heterocyclic nmda/nr2b antagonists

2004
- 2004-05-28 SI SI200430845T patent/SI1648882T1/sl unknown
- 2004-05-28 DE DE602004015610T patent/DE602004015610D1/de not_active Expired - Lifetime
- 2004-05-28 CA CA002527093A patent/CA2527093C/en not_active Expired - Lifetime
- 2004-05-28 MX MXPA05013151A patent/MXPA05013151A/es active IP Right Grant
- 2004-05-28 DK DK04753896T patent/DK1648882T3/da active
- 2004-05-28 ES ES04753896T patent/ES2309540T3/es not_active Expired - Lifetime
- 2004-05-28 EP EP04753896A patent/EP1648882B1/de not_active Expired - Lifetime
- 2004-05-28 JP JP2006515051A patent/JP3927228B2/ja not_active Expired - Lifetime
- 2004-05-28 KR KR1020057023218A patent/KR20060017839A/ko not_active Ceased
- 2004-05-28 AT AT04753896T patent/ATE403651T1/de not_active IP Right Cessation
- 2004-05-28 WO PCT/US2004/017175 patent/WO2004108705A1/en not_active Ceased
- 2004-05-28 AU AU2004245522A patent/AU2004245522B2/en not_active Expired
- 2004-05-28 HR HR20080490T patent/HRP20080490T3/xx unknown
- 2004-05-28 RU RU2005137704/04A patent/RU2339630C2/ru not_active IP Right Cessation
- 2004-05-28 UA UAA200511411A patent/UA81319C2/uk unknown
- 2004-05-28 BR BRPI0410837-0A patent/BRPI0410837A/pt not_active IP Right Cessation
- 2004-05-28 CN CNA2004800153228A patent/CN1798744A/zh active Pending
- 2004-05-28 PT PT04753896T patent/PT1648882E/pt unknown
- 2004-05-28 PL PL04753896T patent/PL1648882T3/pl unknown
- 2004-05-31 MY MYPI20042091A patent/MY138547A/en unknown
- 2004-05-31 AR ARP040101878A patent/AR044579A1/es unknown
- 2004-06-01 PE PE2004000552A patent/PE20050245A1/es not_active Application Discontinuation
- 2004-06-03 TW TW093115972A patent/TW200510378A/zh unknown
- 2004-06-03 CL CL200401365A patent/CL2004001365A1/es unknown
2005
- 2005-11-07 ZA ZA200509000A patent/ZA200509000B/en unknown
- 2005-11-07 IS IS8117A patent/IS8117A/is unknown
- 2005-11-28 MA MA28626A patent/MA27781A1/fr unknown
- 2005-11-29 EC EC2005006192A patent/ECSP056192A/es unknown
- 2005-11-30 CO CO05121658A patent/CO5700762A2/es not_active Application Discontinuation
2006
- 2006-01-03 NO NO20060020A patent/NO20060020L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
MA27781A1 (fr)	2006-02-01
AR044579A1 (es)	2005-09-21
CA2527093A1 (en)	2004-12-16
CN1798744A (zh)	2006-07-05
TW200510378A (en)	2005-03-16
AU2004245522B2 (en)	2009-10-29
WO2004108705A1 (en)	2004-12-16
EP1648882B1 (de)	2008-08-06
MXPA05013151A (es)	2006-03-17
PT1648882E (pt)	2008-10-20
ECSP056192A (es)	2006-04-19
JP2006526650A (ja)	2006-11-24
PL1648882T3 (pl)	2008-12-31
DE602004015610D1 (de)	2008-09-18
MY138547A (en)	2009-06-30
CA2527093C (en)	2009-10-20
NO20060020L (no)	2006-03-03
UA81319C2 (en)	2007-12-25
RU2005137704A (ru)	2006-05-27
KR20060017839A (ko)	2006-02-27
DK1648882T3 (da)	2008-11-24
JP3927228B2 (ja)	2007-06-06
ATE403651T1 (de)	2008-08-15
HRP20080490T3 (en)	2008-11-30
ZA200509000B (en)	2006-12-27
CO5700762A2 (es)	2006-11-30
SI1648882T1 (sl)	2009-02-28
PE20050245A1 (es)	2005-04-13
BRPI0410837A (pt)	2006-06-27
RU2339630C2 (ru)	2008-11-27
CL2004001365A1 (es)	2005-05-06
IS8117A (is)	2005-11-07
EP1648882A1 (de)	2006-04-26
AU2004245522A1 (en)	2004-12-16

Publication	Publication Date	Title
ES2309540T3 (es)	2008-12-16	3-fluoropiperidinas como antagonistas de nmda/nr2b.
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